Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck

…, VE Marquez, ZH Li, JB Bolen, I Stefanova…

Index: Burke Jr.; Lim; Marquez; Li; Bolen; Stefanova; Horak Journal of Medicinal Chemistry, 1993 , vol. 36, # 4 p. 425 - 432

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Citation Number: 94

Abstract

A study was undertaken to prepare inhibitors of the lymphocyte protein-tyrosine kinase p56lCk. Using the known p561ck inhibitor 3, 4-dihydroxy-a-cyanocinnamamide (4) as a lead compound, bicyclic analogues were designed as conformationally constrained mimetics in which the phenyl ring and vinyl side chain of the cinnamamide are locked into a coplanar orientation. Such planarity was rationalized to be an important determinant for binding ...